Effect of hydration on the structure of non aqueous ethyl cellulose/propylene glycol dicaprylate gels

Abstract

Changes in the structural properties of ethyl cellulose/propylene glycol dicaprylate systems (EC/PGD), intended for topical drug delivery, upon addition of water were investigated. Although designed to be a non-aqueous vehicle for moisture sensitive drugs, these systems are expected to experience an aqueous environment during production, storage and application on the skin. Hence, the interaction of water molecules with the non aqueous gel system and their distribution within the gel network is of interest and critical to its application. Experimental techniques of this study were small-deformation dynamic oscillation in shear, modulated differential scanning calorimetry (MDSC), 2H NMR spectroscopy, ATR-infrared spectroscopy, wide-angle X-ray diffraction patterns and light microscopy. Rheological profiles of the gels containing moisture from 0.1 to 40.0% (w/w) deviated considerably from that of the non aqueous system at levels of water above 10.0% in preparations. Gradual replacement of the EC/PGD dipole interactions with stronger hydrogen bonding between ethyl cellulose chains, as the level of hydration increased, contributed to these observations. Formation of clusters of ethyl cellulose, observed under a light microscope, was thus ensued. X-ray diffraction patterns showed that the rearrangement of the polymer chains led to the loss of liquid crystal structures found in the anhydrous gel. MDSC and 2H NMR were used to further shed light on the thermodynamic state of added water molecules in the gels. Plots of enthalpy obtained calorimetrically and a good correlation between MDSC and 2H NMR data indicate that gels with less than two percent hydration contain water in a non-freezable bound state, whereas freezable moieties are obtained at levels of hydration above five percent in composite (EC/PGD/water) gels. © 2012.